4SC-202 - CAS 1186222-89-8
Catalog number:
1186222-89-8
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
Inquire
Targets:
HDAC
Description:
4SC-202 is an orally bioavailable benzamide and inhibitor of human class I histone deacetylases (HDACs) isoenzymes 1, 2 and 3, with potential antineoplastic activity. HDAC inhibitor 4SC-202 selectively binds to and inhibits class I HDACs leading to an accumulation of highly acetylated histones.This may inhibit tumor cell proliferation in susceptible tumor cells. HDACs, upregulated in many tumor types, are a class of enzymes that deacetylate chromatin histone proteins.
Publictions citing BOC Sciences Products
  • >> More
Purity:
0.98
Appearance:
Solid powder
MSDS:
Inquire
Current Developer:
4SC AG
1.Pre-clinical characterization of 4SC-202, a novel class I HDAC inhibitor, against colorectal cancer cells.
Zhijun H1,2, Shusheng W3, Han M4, Jianping L1,2, Li-Sen Q5, Dechun L6. Tumour Biol. 2016 Feb 1. [Epub ahead of print]
Histone deacetylase (HDAC) overactivity in colorectal cancer (CRC) promotes cancer progression. In the current study, we showed that 4SC-202, a novel class I HDAC inhibitor (HDACi), potently inhibited survival and proliferation of primary human colon cancer cells and established CRC lines (HT-29, HCT-116, HT-15, and DLD-1). Yet, the same 4SC-202 treatment was non-cytotoxic to colon epithelial cells where HDAC-1/-2 expressions were extremely low. 4SC-202 provoked apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviated 4SC-202-exerted cytotoxicity in CRC cells. Meanwhile, 4SC-202 induced dramatic G2-M arrest in CRC cells. Further studies showed that AKT activation might be an important resistance factor of 4SC-202. 4SC-202-induced cytotoxicity was dramatically potentiated with serum starvation, AKT inhibition (by perifosine or MK-2206), or AKT1-shRNA knockdown in CRC cells. On the other hand, exogenous expression of constitutively active AKT1 (CA-AKT1) decreased the sensitivity by 4SC-202 in HT-29 cells.
2.4SC-202 activates ASK1-dependent mitochondrial apoptosis pathway to inhibit hepatocellular carcinoma cells.
Fu M1, Wan F2, Li Z3, Zhang F4. Biochem Biophys Res Commun. 2016 Mar 4;471(2):267-73. doi: 10.1016/j.bbrc.2016.01.030. Epub 2016 Jan 8.
The aim of the present study is to investigate the potential anti-hepatocellular carcinoma (HCC) cell activity by 4SC-202, a novel class I HDAC inhibitor (HDACi). The associated signaling mechanisms were also analyzed. We showed that 4SC-202 treatment induced potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. Further, adding 4SC-202 in HCC cells activated mitochondrial apoptosis pathway, which was evidenced by mitochondrial permeability transition pore (mPTP) opening, cytochrome C cytosol release and caspase-3/-9 activation. Inhibition of this apoptosis pathway, by caspase-3/-9 inhibitors, mPTP blockers, or by shRNA-mediated knockdown of cyclophilin-D (Cyp-D, a key component of mPTP), significantly attenuated 4SC-202-induced HCC cell death and apoptosis. Reversely, over-expression of Cyp-D enhanced 4SC-202's sensitivity in HCC cells.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related HDAC Products


CAS 1339928-25-4 CUDC-907

CUDC-907
(CAS: 1339928-25-4)

CUDC-907 is an orally bioavailable inhibitor of both phosphoinositide 3-kinase (PI3K) class I and pan histone deacetylase (HDAC) enzymes, with potential antineo...

CAS 949912-58-7 Remodelin

Remodelin
(CAS: 949912-58-7)

Remodelin, a 2-thiazolylhydrazone derivative, is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10, which acetylates both histones ...

CAS 866323-14-0 Belinostat

Belinostat
(CAS: 866323-14-0)

Belinostat is a novel pan-HDAC inhibitor with IC50 of 27 nM, with activity demonstrated in cisplatin-resistant tumors. It inhibits the growth of tumor cells wit...

CAS 1187075-34-8 Resminostat hydrochloride

Resminostat hydrochloride
(CAS: 1187075-34-8)

Resminostat is an inhibitor of histone deacetylase (HDAC) with IC50 values of 42.5nM, 50.1nM and 71.8nM, respectively against HDAC1, 3 and 6. As an inhibitor of...

CAS 112522-64-2 Tacedinaline

Tacedinaline
(CAS: 112522-64-2)

Tacedinaline, also known as CI-944, is an orally bioavailable substituted benzamide derivative with potential antineoplastic activity. Tacedinaline inhibits his...

CAS 497833-27-9 Givinostat

Givinostat
(CAS: 497833-27-9)

Givinostat (INN) or gavinostat, aslo known as ITF2357,  is a histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic...

CAS 1403783-31-2 Nexturastat A

Nexturastat A
(CAS: 1403783-31-2)

Nexturastat A is an aryl urea derivative that acts as a potent and highly selective inhibitor of histone deacetylase 6 (HDAC6) (IC50= 5.02 +/- 0.60 nM). Nextura...

CAS 149647-78-9 Vorinostat

Vorinostat
(CAS: 149647-78-9)

Vorinostat (suberoylanilide hydroxamic acid, SAHA) is an HDAC inhibitor with IC50 of ~10 nM.

CAS 404951-53-7 Dacinostat

Dacinostat
(CAS: 404951-53-7)

Dacinostat, also known as LAQ824, is a hydroxamate histone deacetylase inhibitor with potential anticancer activity. LAQ824 sensitized nonsmall cell lung cancer...

CAS 287383-59-9 Scriptaid

Scriptaid
(CAS: 287383-59-9)

Scriptaid is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3.

NCC-149
(CAS: 1316652-41-1)

NCC149 is a potent and selective histone deacetylase 8 (HDAC8) inhibitor.

CAS 1622921-15-6 Remodelin

Remodelin
(CAS: 1622921-15-6)

Remodelin, via inhibition of NAT10, mediates nuclear shape rescue of LMNA depleted cells by microtubule reorganization, and improves nuclear shape and fitness o...

CAS 151720-43-3 Oxamflatin

Oxamflatin
(CAS: 151720-43-3)

Oxamflatin, also known as Metacept-3, an aromatic sulfonamide derivative, is a cell-permeable, potent HDAC inhibitor (IC50= 15.7 nM) with antitumor effect.

CAS 875320-29-9 Quisinostat

Quisinostat
(CAS: 875320-29-9)

Quisinostat, also known as JNJ-26481585, is an orally bioavailable, second-generation, hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potent...

CAS 410536-97-9 Sirtinol

Sirtinol
(CAS: 410536-97-9)

Sirtinol is a SIRT inhibitor. Sirtinol significantly increased the acetylation of p53, which has been reported to be a target of SIRT1/2. Sirtinol significantly...

CAS 537034-17-6 BML-210

BML-210
(CAS: 537034-17-6)

BML-210 is a Histone deacetylase (HDAC) inhibitor (IC50 = 87 μM), inducingchanges in gene expression profile.

HDAC-IN-1
(CAS: 1239610-44-6)

HDAC-IN-1, an analogue of MC 1568, is a Iia HDACs inhibitor that could probably influence myogenesis and adipogenesis.

CAS 1215493-56-3 RG2833

RG2833
(CAS: 1215493-56-3)

RGFP 109 is a histone deacetylase (HDAC) inhibitor that has shown to reverse FXN gene silencing in short-term studies of Friedreich ataxia (FRDA) patient cells.

CAS 1069-66-5 Valproic acid sodium salt (Sodium valproate)

Valproic acid sodium salt (Sodium valpro
(CAS: 1069-66-5)

Valproic acid is a HDAC inhibitor by selectively inducing proteasomal degradation of HDAC2, used in the treatment of epilepsy, bipolar disorder and prevention o...

ACY-775
(CAS: 1375466-18-4)

ACY-775 is a selective Histone Deacetylase 6 (HDAC6) inhbiitor with low nanomolar potency and a selectivity of 60- to 1500-fold over class I HDACs. ACY-775 has...

Chemical Structure

CAS 1186222-89-8 4SC-202

Quick Inquiry

Verification code

Featured Items